Department of Chemistry, Changzhi University, Changzhi, Shanxi 046011, China.
University of Michigan Medical School, Ann Arbor, MI 48109, USA.
Molecules. 2020 Mar 5;25(5):1162. doi: 10.3390/molecules25051162.
A series of benzimidazole-derived chalcones containing aromatic amide substituent were designed and synthesized. All of the chalcone compounds were tested for their in vitro antitumor activity against human cancer cell lines (HCT116, HepG2, A549, and CRL-5908). The antiproliferative activity of compounds , , , , , against HCT116 cells was significantly better than that that of 5-Fluorouracil (IC50: 94.63 µM). The antitumor activity of these compounds showed obvious differences between the wild type HCT116 and mutant HCT116 () cells. A preliminary mechanistic study suggested that these compounds act by upregulating the expression of protein in tumor cells without inhibiting the MDM2- interaction.
设计并合成了一系列含有芳香酰胺取代基的苯并咪唑类查尔酮。所有的查尔酮化合物都进行了体外抗肿瘤活性测试，针对人癌细胞系（HCT116、HepG2、A549 和 CRL-5908）。化合物 、 、 、 、 对 HCT116 细胞的增殖抑制活性明显优于 5-氟尿嘧啶（IC50：94.63 µM）。这些化合物的抗肿瘤活性在野生型 HCT116 和突变型 HCT116 () 细胞之间表现出明显的差异。初步的机制研究表明，这些化合物通过上调肿瘤细胞中 蛋白的表达来发挥作用，而不抑制 MDM2- 相互作用。
